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h5-HT(1B) receptor-mediated constitutive Galphai3-protein activation in stably transfected Chinese hamster ovary cells: an antibody capture assay reveals protean efficacy of 5-HT.稳定转染的中国仓鼠卵巢细胞中5-羟色胺（5-HT）（1B）受体介导的组成型Gαi3蛋白激活：抗体捕获分析揭示了5-羟色胺的多种效应
Br J Pharmacol. 2003 Mar;138(6):1077-84. doi: 10.1038/sj.bjp.0705140.
2
Constitutive activity at serotonin 5-HT(1D) receptors: detection by homologous GTPgammaS versus [(35)S]-GTPgammaS binding isotherms.5-羟色胺5-HT(1D)受体的组成性活性：通过同源GTPγS与[(35)S]-GTPγS结合等温线进行检测
Neuropharmacology. 2001;40(1):57-64. doi: 10.1016/s0028-3908(00)00104-0.
3
Antibody capture assay reveals bell-shaped concentration-response isotherms for h5-HT(1A) receptor-mediated Galpha(i3) activation: conformational selection by high-efficacy agonists, and relationship to trafficking of receptor signaling.抗体捕获分析揭示了h5-HT(1A)受体介导的Gα(i3)激活呈钟形浓度-反应等温线：高效激动剂的构象选择及其与受体信号转导的关系。
Mol Pharmacol. 2002 Sep;62(3):590-601. doi: 10.1124/mol.62.3.590.
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Inverse agonism and constitutive activity as functional correlates of serotonin h5-HT(1B) receptor/G-protein stoichiometry.反向激动作用和组成性活性作为5-羟色胺5-HT(1B)受体/G蛋白化学计量学的功能关联
Mol Pharmacol. 2000 Nov;58(5):1042-9. doi: 10.1124/mol.58.5.1042.
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5-HT-stimulated [35S]guanosine-5'-O-(3-thio)triphosphate binding as an assay for functional activation of G proteins coupled with 5-HT1B receptors in rat striatal membranes.5-羟色胺刺激的[35S]鸟苷-5'-O-(3-硫代)三磷酸结合作为大鼠纹状体膜中与5-羟色胺1B受体偶联的G蛋白功能激活的一种检测方法。
Naunyn Schmiedebergs Arch Pharmacol. 2006 Feb;372(5):335-45. doi: 10.1007/s00210-006-0041-x. Epub 2006 Feb 21.
6
Differential activation of Gq/11 and Gi(3) proteins at 5-hydroxytryptamine(2C) receptors revealed by antibody capture assays: influence of receptor reserve and relationship to agonist-directed trafficking.抗体捕获分析揭示5-羟色胺（2C）受体上Gq/11和Gi(3)蛋白的差异激活：受体储备的影响及与激动剂导向转运的关系
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SB-224289--a novel selective (human) 5-HT1B receptor antagonist with negative intrinsic activity.SB - 224289——一种新型的具有负性内在活性的选择性（人）5 - 羟色胺1B受体拮抗剂。
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Reconstitution of the human 5-HT(1D) receptor-G-protein coupling: evidence for constitutive activity and multiple receptor conformations.人5-羟色胺（5-HT）1D受体与G蛋白偶联的重组：组成型活性和多种受体构象的证据
Mol Pharmacol. 2000 Jun;57(6):1132-41.
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Differential modulation by GTPgammaS of agonist and inverse agonist binding to h5-HT(1A) receptors revealed by [3H]-WAY100,635.通过[3H]-WAY100,635揭示GTPγS对激动剂和反向激动剂与h5-HT(1A)受体结合的差异调节作用。
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Agonist and antagonist actions of antipsychotic agents at 5-HT1A receptors: a [35S]GTPgammaS binding study.抗精神病药物对5-HT1A受体的激动和拮抗作用：一项[35S]GTPγS结合研究。
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How much do we know about the coupling of G-proteins to serotonin receptors?我们对G蛋白与血清素受体的偶联了解多少？
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本文引用的文献

1
Antibody capture assay reveals bell-shaped concentration-response isotherms for h5-HT(1A) receptor-mediated Galpha(i3) activation: conformational selection by high-efficacy agonists, and relationship to trafficking of receptor signaling.抗体捕获分析揭示了h5-HT(1A)受体介导的Gα(i3)激活呈钟形浓度-反应等温线：高效激动剂的构象选择及其与受体信号转导的关系。
Mol Pharmacol. 2002 Sep;62(3):590-601. doi: 10.1124/mol.62.3.590.
2
Differential activation of Gq/11 and Gi(3) proteins at 5-hydroxytryptamine(2C) receptors revealed by antibody capture assays: influence of receptor reserve and relationship to agonist-directed trafficking.抗体捕获分析揭示5-羟色胺（2C）受体上Gq/11和Gi(3)蛋白的差异激活：受体储备的影响及与激动剂导向转运的关系
Mol Pharmacol. 2002 Sep;62(3):578-89. doi: 10.1124/mol.62.3.578.
3
Evidence for protean agonism of RX 831003 at alpha 2A-adrenoceptors by co-expression with different G alpha protein subunits.通过与不同的Gα蛋白亚基共表达，RX 831003对α2A肾上腺素能受体具有多变激动作用的证据。
Neuropharmacology. 2002 May;42(6):855-63. doi: 10.1016/s0028-3908(01)00201-5.
4
Histamine H3-receptor-mediated [35S]GTP gamma[S] binding: evidence for constitutive activity of the recombinant and native rat and human H3 receptors.组胺H3受体介导的[35S]GTPγ[S]结合：重组及天然大鼠和人类H3受体组成性活性的证据
Br J Pharmacol. 2002 Jan;135(2):383-92. doi: 10.1038/sj.bjp.0704490.
5
Inverse agonist properties of antipsychotic agents at cloned, human (h) serotonin (5-HT)(1B) and h5-HT(1D) receptors.抗精神病药物在克隆的人5-羟色胺（5-HT）（1B）和人5-HT（1D）受体上的反向激动剂特性
Neuropsychopharmacology. 2001 Sep;25(3):410-22. doi: 10.1016/S0893-133X(01)00237-8.
6
Monovalent anions differentially modulate coupling of the beta2-adrenoceptor to G(s)alpha splice variants.单价阴离子对β2 -肾上腺素能受体与G(s)α剪接变体的偶联有不同的调节作用。
J Pharmacol Exp Ther. 2001 Aug;298(2):840-7.
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Neuromodulation of Na+ channels: an unexpected form of cellular plasticity.钠离子通道的神经调节：一种意想不到的细胞可塑性形式。
Nat Rev Neurosci. 2001 Jun;2(6):397-407. doi: 10.1038/35077553.
8
Constitutive activity at serotonin 5-HT(1D) receptors: detection by homologous GTPgammaS versus [(35)S]-GTPgammaS binding isotherms.5-羟色胺5-HT(1D)受体的组成性活性：通过同源GTPγS与[(35)S]-GTPγS结合等温线进行检测
Neuropharmacology. 2001;40(1):57-64. doi: 10.1016/s0028-3908(00)00104-0.
9
Inverse agonism and constitutive activity as functional correlates of serotonin h5-HT(1B) receptor/G-protein stoichiometry.反向激动作用和组成性活性作为5-羟色胺5-HT(1B)受体/G蛋白化学计量学的功能关联
Mol Pharmacol. 2000 Nov;58(5):1042-9. doi: 10.1124/mol.58.5.1042.
10
Coupling of canine serotonin 5-HT(1B) and 5-HT(1D) receptor subtypes to the formation of inositol phosphates by dual interactions with endogenous G(i/o) and recombinant G(alpha15) proteins.犬5-羟色胺5-HT(1B)和5-HT(1D)受体亚型通过与内源性G(i/o)和重组G(α15)蛋白的双重相互作用与肌醇磷酸形成的偶联。
J Neurochem. 2000 Sep;75(3):1180-9. doi: 10.1046/j.1471-4159.2000.0751180.x.

稳定转染的中国仓鼠卵巢细胞中5-羟色胺（5-HT）（1B）受体介导的组成型Gαi3蛋白激活：抗体捕获分析揭示了5-羟色胺的多种效应

h5-HT(1B) receptor-mediated constitutive Galphai3-protein activation in stably transfected Chinese hamster ovary cells: an antibody capture assay reveals protean efficacy of 5-HT.

作者信息

Newman-Tancredi Adrian, Cussac Didier, Marini Laetitia, Touzard Manuelle, Millan Mark J

机构信息

Department of Psychopharmacology, Institut de Recherches Servier, 125, Chemin de Ronde, Croissy-sur-Seine, Paris 78290, France.

出版信息

Br J Pharmacol. 2003 Mar;138(6):1077-84. doi: 10.1038/sj.bjp.0705140.

DOI:10.1038/sj.bjp.0705140
PMID:12684263
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC1573751/
Abstract
  1. Serotonin 5-HT(1B) receptors couple to G-proteins of the Gi/o family. However, their activation of specific G-protein subtypes is poorly characterised. Using an innovative antibody capture/guanosine-5'-0-(3-[(35)S]thio)-triphosphate ([(35)S]GTPgammaS) binding strategy, we characterised Galpha(i3) subunit activation by h5-HT(1B) receptors stably expressed in Chinese hamster ovary (CHO) cells. 2. The agonists, 5-HT, alniditan and BMS181,101, stimulated Galpha(i3), whereas methiothepin and SB224,289 behaved as inverse agonists. The selective 5-HT(1B) receptor ligand, S18127, modestly stimulated Galpha(i3) and reversed the actions of both 5-HT and methiothepin. S18127 (1 micro M) also produced parallel, dextral shifts of the 5-HT and methiothepin isotherms. 3. Isotopic dilution experiments ([(35)S]GTPgammaS versus GTPgammaS) revealed high-affinity [(35)S]GTPgammaS binding to Galpha(i3) subunits in the absence of receptor ligands indicating constitutive activity. High-affinity [(35)S]GTPgammaS binding was increased 2.8-fold by 5-HT with an increase in the affinity of GTPgammaS for Galpha(i3) subunits. In contrast, methiothepin halved the number of high-affinity binding sites and decreased their affinity. 4. h5-HT(1B) receptor-mediated Galpha(i3) subunit activation was dependent on the concentration of NaCl. At 300 mM, 5-HT stimulated [(35)S]GTPgammaS binding, basal Galpha(i3) activation was low and methiothepin was inactive. In contrast, at 10 mM NaCl, basal activity was enhanced and the inverse agonist activity of methiothepin was accentuated. Under these conditions, 5-HT decreased Galpha(i3) activation. 5. In conclusion, at h5-HT(1B) receptors expressed in CHO cells: (i) inverse agonist induced inhibition of Galpha(i3), and its reversal by S18127, reveals constitutive activation of this Galpha subunit; (ii) constitutive Galpha(i3) activation can be quantified by isotopic dilution [(35)S]GTPgammaS binding and (iii) decreasing NaCl concentrations enhances Galpha(i3) activation and leads to protean agonist properties of 5-HT: that is a switch to inhibition of Galpha(i3).
摘要
  1. 血清素5-HT(1B)受体与Gi/o家族的G蛋白偶联。然而，它们对特定G蛋白亚型的激活情况却鲜为人知。我们采用一种创新的抗体捕获/鸟苷-5'-O-(3-[(35)S]硫代)-三磷酸([(35)S]GTPγS)结合策略，对稳定表达于中国仓鼠卵巢(CHO)细胞中的h5-HT(1B)受体介导的Gα(i3)亚基激活进行了表征。2. 激动剂5-HT、阿尼西坦和BMS181,101可刺激Gα(i3)，而甲硫噻庚因和SB224,289则表现为反向激动剂。选择性5-HT(1B)受体配体S18127适度刺激Gα(i3)，并逆转了5-HT和甲硫噻庚因的作用。S18127(1μM)还使5-HT和甲硫噻庚因的等温线产生平行的右旋位移。3. 同位素稀释实验([(35)S]GTPγS与GTPγS)显示，在无受体配体的情况下，[(35)S]GTPγS与Gα(i3)亚基具有高亲和力结合，表明存在组成性活性。5-HT可使[(35)S]GTPγS与Gα(i3)亚基的高亲和力结合增加2.8倍，并增加GTPγS对Gα(i3)亚基的亲和力。相反，甲硫噻庚因使高亲和力结合位点数量减半，并降低其亲和力。4. h5-HT(1B)受体介导的Gα(i3)亚基激活依赖于NaCl浓度。在300 mM时，5-HT刺激[(35)S]GTPγS结合，基础Gα(i3)激活较低，甲硫噻庚因无活性。相反，在10 mM NaCl时，基础活性增强，甲硫噻庚因的反向激动剂活性增强。在这些条件下，5-HT降低Gα(i3)激活。5. 总之，在CHO细胞中表达的h5-HT(1B)受体：(i)反向激动剂诱导的Gα(i3)抑制及其被S18127逆转，揭示了该Gα亚基的组成性激活；(ii)组成性Gα(i3)激活可通过同位素稀释[(35)S]GTPγS结合进行定量；(iii)降低NaCl浓度可增强Gα(i3)激活，并导致5-HT具有多变的激动剂特性：即转变为抑制Gα(i3)。